Anti-calculus dental composition

ABSTRACT

The present invention relates generally to an anti-calculus composition and method for treating subgingival calculus. The anti-calculus composition comprises a pyrophosphate and a tripolyphosphate in a pharmaceutically acceptable carrier. The composition may also comprise a fluoride providing compound.

CROSS-REFERENCE

This application is a divisional application of U.S. patent applicationSer. No. 11/644,618 filed Dec. 22, 2006, the content of which is herebyincorporated by reference in its entirety.

FIELD OF THE INVENTION

The present invention relates generally to anti-calculus compositionsand methods for the treatment of a dental disease in a subject bypreventing, reducing, or removing dental calculus.

BACKGROUND OF THE INVENTION

Dental Plaque

Dental plaque is a biofilm (usually a pale yellow to white color) thatbuilds up on the surface of teeth. If not removed regularly, it can leadto dental cavities (caries) or periodontal problems (such asgingivitis). The microorganisms that form the biofilm are almostentirely bacteria (mainly streptococcus and anaerobes), with thecomposition varying by location in the mouth. The microorganisms presentin dental plaque are all naturally present in the oral cavity, and arenormally harmless. However, failure to remove plaque allows it to buildup in a thick layer and leads to increased bacterial growth.

Dental Calculus

Dental plaque is a precursor of calculus. Dental calculus, or tartar,refers to a build-up of hardened (mineralized) plaque on the teeth,formed by the presence of saliva, debris, and minerals. Mature calculusconsists of an inorganic portion which is largely calcium phosphatearranged in a hydroxyapatite crystal lattice structure similar to bone,enamel, and dentine. An organic portion is also present and consists ofdesquamated epithelial cells, leukocytes, salivary sediment, fooddebris, and various types of microorganisms. Its rough surface providesan ideal medium for bacterial growth, threatening the health of the gumsand absorbing unaesthetic stains far more easily than natural teeth.

Calculus comes in two forms. Supragingival (outside the gums) calculusis the visible deposit that forms on the top of the teeth. Subgingival(inside the gums) calculus forms in pockets between teeth and gums.Subgingival calculus is more harmful as it facilitates faster growth ofbacteria.

Buildup of calculus often causes swelling, bleeding and weakening ofgums, and can lead to gum recession and tooth loss. Calculus can evenextend into pockets created between the tooth and gums. The anaerobicbacteria found in pockets around teeth may be linked to cardiovasculardisease and pre-term low birth weight babies. These pockets aredifficult to reach by tooth brushing, and are not affected by standardmouthwashes.

Calculus accumulates in the absence of proper oral care. Once formed, itcan be removed currently only by professional cleaning by a dentist ordental hygienist using a scaling procedure, which is a process involvingmetal scrapers to mechanically remove calculus from tooth surfaces. Themechanical dental scaling procedure may be effective in calculusremoval. However, this procedure has several disadvantages. Onedisadvantage of dental scaling is that the process can destroy dentalcementum, which is a tooth formation critical to gum/tooth attachment.Another disadvantage of dental scaling is that the treatment may removehealthy gum tissue, which cannot regenerate. Still another disadvantageis that the procedure is painful.

A variety of chemical and biological agents have also been suggested toretard calculus formation or to remove calculus after it is formed.Pyrophosphate salts and other chemical agents are known to have theability to retard calculus formation. For example, in U.S. Pat. Nos.4,999,184 and 4,610,871, the use of monoalkyl or dialkyl ethers ofdianhydrohexitols to inhibit the formation of plaque and calculus onteeth is described. U.S. Pat. No. 4,178,363 describes the use ofn-undecylenic fatty acid or a calcium or zinc salt thereof for reducingdental plaque and infections of the teeth and gums. U.S. Pat. No.4,119,711 describes spiro 1-(hydroxyalkyl)-piperidino derivatives whichhave efficacy in reducing the formation of plaque. Additionally, U.S.Pat. No. 3,887,712 discloses that alexidine dihydrofluoride is useful inthe treatment of dental plaque, calculus, gingivitis and relatedperiodontal diseases. U.S. Pat. No. 4,160,821 discloses that a glycerinsolution of zinc chloride or other acceptable zinc salts provideseffective therapy for gingivitis when applied to the gingival and teeth.U.S. Pat. No. 4,060,600 teaches a method of treating teeth in dentistry,for the prevention of calculus, removal of caries, and dissolution ofplaque, comprising applying an aqueous solution containing ahypochlorite of an alkali and/or alkaline earth metal, and an aminocompound capable of forming water-soluble non-mucous irritating N-chloroand/or N-dichloro derivatives thereof to the teeth. However, all ofthese chemical and biological agents have some disadvantages, such asdiscoloration of teeth or tongue, desquamation and soreness of oralmucosa, objectionable taste, toxicity, and may also causes an imbalanceof the oral flora.

Dental Pockets and Gum Disease

Calculus if not properly removed may lead to more serious dentalproblems such as dental pocket formation and gum disease. Calculusformations house bacteria which excrete toxins that erode periodontalligament connections, leading to erosion of periodontal ligamentconnections. This erosion separates teeth from gums, forming dental“pockets.” The pockets facilitate further calculus growth, leading tofurther separation of the teeth from the gums, ending in tooth loss.

According, there is a need for effective anti-calculus compositions andmethods for the treatment of dental diseases via the non-mechanicalremoval of calculus from tooth surfaces, without the disadvantages thatare commonly associated with conventional treatments. The anti-calculuscomposition of the present invention is very effective in removal ofsubgingival calculus, which leads to reduction of dental pockets and gumdisease, and to healthier gums and prevent tooth loss.

SUMMARY OF THE INVENTION

In accordance with the present invention, an anti-calculus compositionis provided for the treatment of a dental disease in a subject bypreventing, reducing, or removing dental calculus. In one embodiment,the anti-calculus composition comprises two or more anti-calculusagents. The anti-calculus agents each are a polyphosphate. When theanti-calculus composition comprises two anti-calculus agents, the firstanti-calculus agent is a pyrophosphate, including pyrophosphoric acidand a pharmaceutically acceptable salt thereof; the second anti-calculusagent is a tripolyphosphate, including tripolyphosphoric acid and apharmaceutically acceptable salt thereof.

In another embodiment, the anti-calculus composition further comprisesone or more pharmaceutically acceptable carriers. The anti-calculuscomposition may comprise a C₂-C₂₀ organic acid, such as citric acid, andbicarbonate, such as an alkali bicarbonate. The anti-calculuscomposition may also comprise a fluoride providing compound.

The present invention also provides a method for treating subgingivalcalculus using the anti-calculus composition described herein above. Themethod comprises the steps of applying an effective amount of a solutionor suspension that contains the anti-calculus composition topically tothe oral cavity of the subject, particularly to the teeth and/or gums ofa subject. When the anti-calculus composition is provided in aconcentrated from such as powder or a concentrated solution, the methodmay also include the step of preparing an application composition fromthe anti-calculus composition as a solution or suspension prior to theapplying step.

Further, the present invention also relates to a method for treatingsubgingival calculus in a subgingival pocket, comprising the steps ofpreparing a composition comprising at least one phosphate-containinganti-calculus agent, loading the composition into an applicator devicewith at least one orifice, wherein the device is adapted for delivery ofthe composition through the orifice under pressure; and applying thecomposition to the subgingival pocket.

Other aspects of the invention are described throughout thespecification

DETAILED DESCRIPTION OF THE INVENTION

The present invention relates generally to a dental composition andmethods for the treatment of a dental disease in a subject via theprevention, reduction, and removal of dental calculus. Moreparticularly, the present invention relates to an anti-calculuscomposition that is administered topically to the oral cavity of thesubject Suitable topical composition includes a solution, powder, toothpaste, cream, gel or dentifrice, a mouth wash or rinse, a chewabletablet, a mouth freshener, a toothpick, a dental pack, dental floss, orother dental implements. The anti-calculus composition of the present iseffective in preventing, reducing, and removing calculus, especiallysubgingival calculus, but without the disadvantages that are commonlyassociated with conventional treatments of dental diseases.

To facilitate understanding of the invention set forth in the disclosurethat follows, a number of abbreviations and terms are defined below.Unless defined otherwise, all technical and scientific terms used hereingenerally have the same meaning as commonly understood by one ofordinary skill in the art to which this invention belongs.

The term “teeth” refers to natural teeth and any other hard surfaces,such as crowns, caps, fillings, bridges, dental implants, and the like,that are permanently fixed within the oral cavity and cleansed in situwithin the oral cavity of a subject.

The term “calculus” refers to mineralized dental plaque biofilms.

The term “effective amount” refers to an amount of an agent or agents(e.g., anti-calculus agent or agents) high enough to significantlyimprove the condition to be treated, but low enough to avoid seriousside effects (at a reasonable benefit/risk ratio), within the scope ofsound medical/dental judgment. The safe and effective amount of an agent(e.g., anti-calculus agent or agents) may vary with the particularcondition being treated, the age and physical condition of the patientbeing treated, the severity of the condition, the duration of treatment,the nature of concurrent therapy, and the particular vehicle from whichthe agent is applied.

The term “oral composition” refers to a topical composition that in theordinary course of usage, is not intentionally swallowed for purposes ofsystemic administration of particular agents, but is rather retained inthe oral cavity for a time sufficient to contact substantially theexposed dental surfaces and/or oral tissues for purposes of oralactivity. The oral composition of the present invention may be in theform of a solution, toothpaste, dentifrice, tooth powder, topical oralgel, mouth rinse, mouth wash, denture product, mouthspray, lozenge, oraltablet, or chewing gum.

The term “orally-acceptable carrier” or “pharmaceutically acceptableexcipient” refers to a suitable vehicle, which can be used to apply thepresent anti-calculus compositions to the oral cavity in a safe andeffective manner. Such vehicle may include materials such as fluorideion sources (also known as fluoride providing compounds), additionalanti-calculus agents, buffers, abrasive materials, peroxide sources,alkali metal bicarbonate salts, thickening materials, humectants, water,surfactants, titanium dioxide, flavor system, sweetening agents,xylitol, coloring agents, natural saliva, and mixtures thereof.

The term “pharmaceutically acceptable” refers to those compounds,materials, compositions, and/or dosage forms which are, within the scopeof sound medical judgment, suitable for use in contact with the tissuesof human beings and animals without excessive toxicity, irritation,allergic response, or other problem or complication, commensurate with areasonable benefit/risk ratio.

The term “treating” means preventing, reducing, and/or removing dentalcalculus, thereby preventing, reducing and/or alleviating a dentaldisease.

The term “subgingival” means inside the gums. The anti-calculuscomposition of the present invention enters subgingival spaces orpockets, but it is understood that supragingival calculus can also betreated with the anti-calculus composition of the present invention.

Anti-Calculus Composition

The anti-calculus composition of the present invention for the treatmentof a dental disease, such as subgingival calculus, comprises two or moreanti-calculus agents. Suitable anti-calculus agents include, but are notlimited to, polyphosphates, particularly linear molecularly dehydratedpolyphosphoric acids and pharmaceutically acceptable salts thereof. Theterm “polyphosphate” is used herein in a broad sense, which includes apolyphosphoric acid and pharmaceutically acceptable salts thereof,wholly or partially neutralized. Non-limiting exemplary polyphosphatesare trimetaphosphates, pyrophosphates, tripolyphosphates,tetrapolyphosphates, and hexametaphosphates. Similarly, those phosphateterms also include their corresponding phosphoric acid and various formsof pharmaceutically acceptable salts thereof; wholly or partiallyneutralized. For example, a pyrophosphate includes, but is not limitedto, pyrophosphoric acid, sodium pyrophosphate, di-sodium pyrophosphates,tri-sodium pyrophosphates, tetra-sodium pyrophosphates, potassiumpyrophosphate, di-potassium pyrophosphates, tri-potassium pyrophosphate,and tetra-potassium pyrophosphates. The polyphosphates employed in thepresent invention are all from commercial sources and are readilyavailable from a number of chemical suppliers. In general, theanti-calculus agents each are employed in the instant anti-calculuscomposition in the amount from about 0.1 to about 90%, from about 1 toabout 80%, or from about 2 to about 50% by weight. When theanti-calculus composition is in a concentrated form, the content of eachanti-calculus agent is in the amount from about 10 to about 90%, fromabout 15 to about 80%, or from about 20 to about 50% by weight.

The anti-calculus composition of the present invention also includes oneor more pharmaceutically acceptable carriers. In one exemplaryembodiment, the anti-calculus composition comprises an alkali metalbicarbonate salt, such as sodium bicarbonate or potassium bicarbonate.Alkali metal bicarbonates are soluble in water and unless stabilized,release carbon dioxide in an aqueous solution. When supplied as aconcentrated form, the anti-calculus composition contains from about 2to about 50%, from about 10 to about 40%, or from about 15 to about 30%by weight of an alkali metal bicarbonate.

The anti-calculus composition of the present invention may also have aC2-C20 organic acid, such as citric, malic, lactic, alginic, succinic,tartaric, and ascorbic acids. When supplied in a concentrated form, thelevel of the C₂-C₂₀ organic acid may range in an amount from about 2 toabout 50%, from about 10 to about 40%, or from about 15 to about 30% byweight.

The desired pH range of the anti-calculus composition of the presentinvention is between about 6 and about 9, or between about 7.5 and about8.1. The pH of the present anti-calculus compositions is readilyadjusted via buffering agents.

In an exemplary embodiment of the present invention, the anti-calculuscomposition comprises substantially equal amounts of tetra-potassiumpyrophosphate, sodium tripolyphosphate, sodium bicarbonate, and citricacid.

In another exemplary embodiment, the anti-calculus composition comprisestetra-potassium pyrophosphate in the amount of about 37% by weight,sodium tripolyphosphate in the amount of about 37% by weight, sodiumbicarbonate in the amount of about 12% by weight, citric acid in theamount of 12% by weight and sodium fluoride as a fluoride providingcompound in the amount of about 0.02% by weight.

These two exemplary anti-calculus compositions are readily dissolved inwater, forming an application solution to be applied topically to theoral cavity of a subject. The application solution can be readilyapplied using a common device such as an oral irrigator or sub-gingivaloral applicator.

Formulations and Administration

The anti-calculus composition of the present invention may be formulatedin various forms suitable for topical applications to the oral cavity ofa subject. In one embodiment, the anti-calculus composition isformulated as a dentifrice, which is substantially solid or pasty incharacter, such as tooth powder, a dental tablet, a tooth paste (cream),or a dental gel. Toothpastes (creams) and gels typically contain in thetopical vehicle a natural or synthetic thickener or gelling agent.Additionally, the vehicle of such solid or pasty dentifrice preparationstypically contains an orally or dentally acceptable polishing materialfor use in conjunction with brushing of the teeth. Examples of suchpolishing materials are water-insoluble sodium metaphosphate, potassiummetaphosphate, tri-calcium phosphate, dihydrated calcium phosphate,anhydrous di-calcium phosphate, calcium pyrophosphate, magnesiumorthophosphate, tri-magnesium phosphate, calcium carbonate, aluminumsilicate, zirconium silicate, silica, bentonite, and mixtures thereof.Other suitable polishing materials include the particulate thermosettingresins described in U.S. Pat. No. 4,070,510, such as melamine-,phenolic-, and urea-formaldehydes, and cross-linked polyepoxides andpolyesters. Examples of polishing materials include silica gel orcolloidal silica, and complex amorphous alkali metal alumino-silicates.

In another embodiment, the anti-calculus composition of the presentinvention is formulated as a powder, which is readily dissolved in waterto form a liquid application solution. Because of their ease ofadministration, liquid preparations represent an advantageous oraldosage unit form. Such compositions and preparations should contain atleast 0.1 percent of active compound. The percentage of theanti-calculus composition in these compositions may be varied and mayconveniently be between about 1% to about 20% of the weight of theapplication solution.

In still another embodiment, the anti-calculus composition is providedas a liquid formulation either in a concentrated or ready-to-use form,which can be directly applied or diluted quickly prior to theapplication.

In one embodiment, the invention relates to a method for applying ananti-calculus composition directly to the subgingival pocket using anapplicator device. Such devices include, for example, any commerciallyavailable water pick or oral irrigator, which usually have a very small(less than 100 mm, and usually less than 10 mm, and in particularbetween 5 and 10 mm) orifice that is designed for reaching thesubgingival pocket. Such devices are also usually adapted for applyingthe composition under pressure so that it can be more easily applied(i.e., “squirted”) in an upward direction into the subgingival pocket ofthe upper teeth, in addition to being applied to the subgingival pocketof the lower teeth. In this embodiment, it is also most beneficial toformulate the composition as a semi-solid or gel such that the viscosityof the composition is sufficient to allow it to stay in place in thesubgingival pocket to enhance efficacy (usually more than 5,000; such asbetween 5,000 and 1000,000 centipoise at 20° C.)

Orally Acceptable Carrier

The orally acceptable carrier comprises one or more compatible solid orliquid filler diluents or encapsulating substances which are suitablefor topical oral administration. By “compatible,” as used herein, ismeant that the components of the composition are capable of beingcomingled without interaction in a manner which would substantiallyreduce the composition's stability and/or efficacy.

The carriers or excipients of the present invention can include theusual and conventional components of dentifrices (including non-abrasivegels and gels for subgingival application), mouth rinses, mouth sprays,chewing gums, and lozenges (including breath mints) as more fullydescribed hereinafter.

The choice of a carrier to be used is basically determined by the waythe anti-calculus composition is to be introduced into the oral cavity.If a toothpaste (including tooth gels, etc.) is to be used, then a“toothpaste carrier” is chosen (e.g., abrasive materials, sudsingagents, binders, humectants, flavoring and sweetening agents, etc.) asdisclosed in, e.g., U.S. Pat. No. 3,988,433, to Benedict. If a mouthrinse is to be used, then a “mouth rinse carrier” is chosen (e.g.,water, flavoring and sweetening agents, etc.), as disclosed in, e.g.,U.S. Pat. No. 3,988,433 to Benedict. Similarly, if a mouth spray is tobe used, then a “mouth spray carrier” is chosen or if a lozenge is to beused, then a “lozenge carrier” is chosen (e.g., a candy base), candybases being disclosed in, e.g., U.S. Pat. No. 4,083,955, toGrabenstetter et al.; if a chewing gum is to be used, then a “chewinggum carrier” is chosen (e.g., gum base, flavoring and sweeteningagents), as disclosed in, e.g., U.S. Pat. No. 4,083,955, toGrabenstetter et al. If a sachet is to be used, then a “sachet carrier”is chosen (e.g., sachet bag, flavoring and sweetening agents). If asubgingival gel is to be used (for delivery of actives into theperiodontal pockets or around the periodontal pockets), then a“subgingival gel carrier” is chosen as disclosed in, e.g. U.S. Pat. Nos.5,198,220 and 5,242,910, issued Mar. 30, 1993 and Sep. 7, 1993,respectively both to Damani. Carriers suitable for the preparation ofcompositions of the present invention are well known in the art. Theirselection will also depend on secondary considerations like taste, cost,and shelf stability, etc.

The anti-calculus compositions of the present invention may be in theform of non-abrasive gels, including subgingival gels, which may beaqueous or non-aqueous. Aqueous gels generally include a thickeningagent (from about 0.1% to about 20%), a humectant (from about 10% toabout 55%), a flavoring agent (from about 0.04% to about 2%), asweetening agent (from about 0.1% to about 3%), a coloring agent (fromabout 0.01% to about 0.5%), and the balance water. The anti-calculuscompositions may further comprise a fluoride providing agent (from about0.02% to about 0.3% as fluoride ion).

Compositions of the subject invention may also be in the form ofdentifrices, such as toothpastes, tooth gels and tooth powders.Components of such tooth paste and tooth gels generally include one ormore of a dental abrasive (from about 6% to about 50%), a surfactant(from about 0.5% to about 10%), a thickening agent (from about 0.1% toabout 5%), a humectant (from about 10% to about 55%), a flavoring agent(from about 0.04% to about 2%), a sweetening agent (from about 0.1% toabout 3%), a coloring agent (from about 0.01% to about 0.5%) and water(from about 2% to about 45%). Such tooth paste or tooth gel may alsoinclude one or more of an anticaries agent (from about 0.02% to about0.3% as fluoride ion), and an anti-calculus agent (from about 0.1% toabout 13%). Tooth powders, of course, contain substantially allnon-liquid components.

The anti-calculus composition of the present invention may also beprovided as a mouthwash, including a mouth spray. Components of suchmouthwashes and mouth sprays typically include one or more of water(from about 45% to about 99%), ethanol (no greater than about 25%), ahumectant (no greater than about 50%), a surfactant (no greater thanabout 7%), a flavoring agent (no greater than about 2%), a sweeteningagent (no greater than about 3%), and a coloring agent (no greater thanabout 0.5%). Such mouthwashes and mouth sprays may also include afluoride providing agent (no greater than about 0.3% as fluoride ion).

The anti-calculus composition of the present invention may be providedas dental solutions including irrigation fluids. Components of suchdental solutions generally include one or more of water (from about 90%to about 99%), preservative (from about 0.01% to about 0.5%), thickeningagent (from 0% to about 5%), flavoring agent (from about 0.04% to about2%), sweetening agent (from about 0.1% to about 3%), and surfactant(from 0% to about 5%).

The anti-calculus composition of the present invention may be providedas chewing gum compositions, which typically include one or more of agum base (from about 50% to about 99%), a flavoring agent (from about0.4% to about 2%) and a sweetening agent (from about 0.01% to about20%).

The anti-calculus composition of the present invention may be providedas a dental implement impregnated with the present anti-calculuscomposition. The dental implement comprises an implement for contactwith teeth and other tissues in the oral cavity, said implement beingimpregnated with a composition comprising the present composition. Thedental implement can be impregnated fibers including dental floss ortape, chips or strips and polymer fibers.

A medicated dental floss for controlling, reducing, removing, orpreventing calculus is also contemplated. The floss incorporates theanti-calculus composition of the present invention which, as a result ofthe flossing action, is deposited to the inter-dental area of the teeth.Examples of making such floss are well known and are disclosed forexample in U.S. Pat. No. 5,603,921.

Various other materials may be incorporated in the anti-calculuscomposition of the present invention such as whitening agents,preservatives, silicones, fluorine, anti-inflammatory agents,antioxidants, anti-microbial agents, anti-pain agents, chlorophyllcompounds, excipients, fragrance, colorants and mixtures thereof. Theseadjuvants, where present, are incorporated in the preparations inamounts which do not substantially adversely affect the properties andcharacteristics desired.

Any suitable flavoring or sweetening material may also be employed. Inthe instance where auxiliary sweeteners are utilized, the presentinvention contemplates the inclusion of those sweeteners well known inthe art, including both natural and artificial sweeteners. Examples ofsuitable flavoring constituents are flavoring oils, e.g. oil ofspearmint, peppermint, wintergreen, sassafras, clove, sage, eucalyptus,marjoram, cinnamon, lemon, and orange, and methyl salicylate. Suitablesweetening agents include sucrose, lactose, maltose, dextrose, levulose,sorbitol, xylitol, d-tryptophan, dihydrochalcones, sodium cyclamate,perillartine, APM (aspartyl phenyl alanine, methyl ester), saccharineand the like.

The anti-calculus composition of the present invention may also be usedin combination with other compounds or compositions that may also beuseful in the treatment or amelioration of the diseases or conditionsfor which the anti-calculus compositions of the present invention areuseful. Such other compounds or compositions may be administered, by aroute and in an amount commonly used therefore, contemporaneously orsequentially with the anti-calculus composition of the presentinvention.

The effective amount of the anti-calculus composition of the presentinvention to be employed therapeutically for the treatment of a dentaldisease depends on a number of factors, among which are included,without limitation, the patient's sex, weight and age, the underlyingcauses of the condition or disease to be treated, the formulation, andthe potency of the active component.

Application

In the practice of this invention, the anti-calculus composition isapplied to dental enamel and gums as by mixing with a liquid vehicle,and applied via an orally-acceptable device, such as an oral irrigatoror sub-gingivital applicator. The anti-calculus composition is appliedregularly to dental enamel, such as every day or every other day andpreferably from 1 to 3 times daily, for at least 2 weeks up to 8 weeksor more up to lifetime. The anti-calculus composition is discharged inthe rinsing process and any residual composition may linger in dentalpockets, dissolving calculus, until the next composition applicationwhereas the prior application will be rinsed away.

It should be understood that the application ranges set forth above areexemplary only and are not intended to limit the scope of thisinvention. The therapeutically effective amount of the anti-calculuscomposition may vary with factors including, but not limited to, theefficacy of the composition, stability of the composition, the severityof the conditions to be alleviated, the age and sensitivity of thesubject to be treated, and the like, as will be apparent to a skilledartisan. The amount of administration can also be adjusted as thevarious factors change over time.

Method of Use

The present invention also relates to methods for treating a dentaldisease by preventing, reducing, and removing dental calculus in asubgingival pocket. The method comprises the steps of preparing asolution or suspension from the anti-calculus composition whichcomprises at least a pyrophosphate and polyphosphate in apharmaceutically acceptable carrier and applying the solution orsuspension to the subgingival pocket.

It should be understood that the present invention relates not only tomethods for delivering the present compositions to the oral cavity of ahuman, but also to methods of delivering the composition to the oralcavity of other animals, e.g., household pets or other domestic animals,or animals kept in captivity.

For example, a method of use may include brushing a dog's teeth with theanti-calculus composition. Another example would include the rinsing ofa cat's mouth with the anti-calculus composition for a sufficient amountof time to see a benefit. Pet care products such as chews and toys maybe formulated to contain the present anti-calculus composition. Thecomposition is incorporated into a relatively supple but strong anddurable material such as rawhide, ropes made from natural or syntheticfibers, and polymeric articles made from nylon, polyester orthermoplastic polyurethane. As the animal chews, licks or gnaws theproduct, the incorporated anti-calculus composition is released into theanimal's oral cavity into a salivary medium, comparable to an effectivebrushing or rinsing.

Therapeutic Implications

A number of clinical diseases and conditions may be treated using theanti-calculus composition of the present invention. Subjects who wouldbenefit from treatment with the instant anti-calculus compositionsinclude those who suffer from dental plaque; dental tartar; dentalcalculus; gum disease; dental pockets; dental caries; gingivitis; orperiodontitis.

The present invention also involves a method for treating teeth or gumsto reduce dental calculus, which comprises the step of applying to thesurface of the teeth and/or gums the anti-calculus compositions of thepresent invention as described above. The compositions can be applied tothe teeth and gums by any conventional methods, such as irrigating,brushing, spraying, painting or rinsing of the oral cavity and the like.

It has been found that the anti-calculus composition of the presentinvention is very effective in the treatment of subgingival calculus, inaddition to supragingival calculus. As a result, subgingivalinflammations, previously unmolested by prior art, have been found to beextinguished with the composition of the present invention. Thesubsequent reduction in inflammation provides relief to acute oral paincaused by infection. Further treatment has been found to restore healthy“pink” gum tissue to formally inflamed gums within two weeks. It hasalso been found that in addition to oral inflammation reduction,periodontal pocket reduction occurs in all test subjects. This processof pocket reduction is the result of both upper gum inflammationreduction, and most importantly, dental gum reattachment followingsubgingival calculus elimination.

The following examples are further illustrative of the nature of thepresent invention, but it is understood that the invention is notlimited thereto. All amounts and proportions referred to herein and inthe appended claims are percent by weight.

EXAMPLE

Eleven volunteer subjects with dental calculus, dental pockets withinflammation, and/or periodontal disease, with periodontal pockets, atleast one periodontal pocket in excess of 5 mm, received treatment withthe composition of the invention.

Treatment for 12 subjects began with ⅛ tsp. of the compositionadministered orally using an oral irrigator, in 500 mL of warm water,one to two times a day for 90 days. Improvements in gum inflammationwere noted for all 11 subjects within 7 days as visually examined.Subjects experienced up to a 50% improvement in dental pocket depth bythe end of the treatment. No periodaontal pockets increased, and allinfection in every subject was arrested.

Subject 12, a 55 year old male, under the care of his personal dentist,had been in a quarterly cleaning and perio monitoring regiment for threetears prior to treatment. Periodontal surgery had been indicated priorto treatment with the composition. After a three month treatmentprogram, subject 12's periodontal record improved from 13 bleeding sitesand 21 perio sites in 10 teeth, to 7 bleeding sites and 15 perio sitesin 10 teeth. After an additional three months of treatment, subject 12'speriodontal record further improved to just 4 bleeding sites and 10perio sites in 8 teeth, after which periodontal surgery was no longerindicated.

Subject 13, a 45 year old male at the time of treatment, was in additionto suffering periodontal disease, also suffering from advancedperiodontal disease with pockets in excess of 8 mm. Subject 13 wasexperiencing multiple abscesses, bleeding and pus release with gummassage in 6 pockets. Treatment began, as above, with ⅛ tsp of thecomposition of the invention administered orally using an oralirrigator, in 500 mL of warm water, one to two times a day for 90 days.In addition, six pockets with in excess of 8 mm were treated with ⅛ tspof the composition of the invention, administered orally using asubgingival applicator, in 25 mL warm water, one to two times a day for90 days.

Subject was monitored for inflammation, swelling, infection and pocketdepth every 30 days, with six pockets being recorded. As indicated inTable 1 below, this subject realized significant reduction in dentalpocket depth as well as elimination of oral infection and inflammation.Prior to treatment, the subject had a deep dental pocket depth rangingfrom 7 to 12 mm (Table 1). After treatment for ninety days, dentalpocket depth was reduced to 3 to 8 mm.

TABLE 1 Summary Dental Pocket Depth (mm) Tooth location of Prior to 30days after 60 days after 90 days after dental pocket treatment treatmenttreatment treatment 22 Facial Mesial 12 11 9 8 23 Facial Distal 8 6 4 331 Facial Distal 8 6 5 4 19 Facial Mesial 11 9 7 6 18 Facial Distal 10 98 8 19 Lingual Distal 10 9 9 8

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The information presented above is provided to give those of ordinaryskill in the art with a complete disclosure and description of how tomake and use the embodiments of the invention, and is not intended tolimit the scope of what the inventor regards as his invention.Modifications of the above-described modes for carrying out theinvention that are obvious to persons of skill in the art are intendedto be within the scope of the following claims. All publications,patents, and patent applications cited in this specification areincorporated herein by reference as if each such publication, patent orpatent application were specifically and individually indicated to beincorporated herein by reference.

1. A composition for dissolving subgingival calculus in a subgingivalpocket after formation thereof comprising: a) a pyrophosphate consistingof tetrapotassium pyrophosphate; b) a polyphosphate consisting oftripolyphosphate; c) an alkali metal bicarbonate salt consisting ofsodium bicarbonate; d) a C2-C20 organic acid consisting of citric acid;and e) a fluoride providing compound; wherein the composition iseffective to dissolve subgingival calculus.
 2. The composition of claim1, wherein the fluoride providing compound is sodium fluoride.
 3. Acomposition for dissolving subgingival calculus in a subgingival pocketafter formation thereof comprising: a) from 20% to 40% by weight oftetrapotassium pyrophosphate; b) from 20% to 40% by weight of sodiumtripolyphosphate; c) from 5% to 20% by weight of sodium bicarbonate; d)from 4% to 20% by weight of citric acid; and e) from 0.01 to 1% byweight of sodium fluoride; wherein the composition is effective todissolve subgingival calculus.